Quinone oxidoreductase-2-mediated prodrug cancer therapy.
|Abstract||DNA-damaging agents are widely used in cancer treatment despite their lack of tumor specificity. Human NQO2 (quinone oxidoreductase-2) is an atypical oxidoreductase because no endogenous electron donor has been identified to date. The enzyme converts CB1954 [5-(aziridin-1-yl)-2,4-dinitrobenzamide], in the presence of the synthetic nicotinamide cofactor analog EP0152R, to a cytotoxic bifunctional alkylating agent. NQO2 activity in hepatocellular t ... [truncated at 450 characters in length]|
|Author||Middleton, Mark R; Knox, Richard; Cattell, Emma; et al|
|Subject||Adult Aged Antineoplastic Agents Aziridines Cell Death Cross-Linking Reagents Crystallography, X-Ray DNA, Neoplasm Enzyme Activation Female Humans Male Middle Aged Models, Molecular Neoplasms Prodrugs Quinone Reductases adverse effects chemistry pharmacokinetics therapeutic use adverse effects chemistry pharmacokinetics therapeutic use drug effects pharmacology metabolism drug effects drug therapy chemistry pharmacology therapeutic use chemistry metabolism|